AZD-7687

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 522494

CAS#: 1166827-44-6

Description: AZD7687, a reversible and selective DGAT1 inhibitor with IC50 value of 80 nM. AZD-7687 attenuates postprandial triacylglyceride excursion. AZD7687 markedly reduced postprandial TAG excursion with a steep concentration-effect relationship. Incremental TAG AUC (area under the serum concentration vs. time curve) following SMM 60% was decreased >75% from baseline at doses ≥5 mg (p < 0.0001 vs. placebo). Serum levels of diacylglycerol, specifically measured with mass spectrometry, did not increase after AZD7687 administration. Nausea, vomiting and diarrhoea were reported with increasing doses and they limited dose escalation. Lowering of SMM fat content to 45 or 30% in five cohorts gradually reduced the frequency of gastrointestinal symptoms at a given dose of AZD7687.

Chemical Structure

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AZD-7687
CAS# 1166827-44-6
Instruction

Theoretical Analysis

MedKoo Cat#: 522494
Name: AZD-7687
CAS#: 1166827-44-6
Chemical Formula: C21H25N3O3
Exact Mass: 367.19
Molecular Weight: 367.449
Elemental Analysis: C, 68.64; H, 6.86; N, 11.44; O, 13.06

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Synonym: AZD-7687; AZD 7687; AZD7687.

IUPAC/Chemical Name: 2-((1s,4s)-4-(4-(6-carbamoyl-3,5-dimethylpyrazin-2-yl)phenyl)cyclohexyl)acetic acid

InChi Key: YXFNPRHZMOGREC-GASCZTMLSA-N

InChi Code: InChI=1S/C21H25N3O3/c1-12-19(24-20(21(22)27)13(2)23-12)17-9-7-16(8-10-17)15-5-3-14(4-6-15)11-18(25)26/h7-10,14-15H,3-6,11H2,1-2H3,(H2,22,27)(H,25,26)/t14-,15+

SMILES Code: OC(C[C@H]1CC[C@@H](C2=CC=C(C3=C(C)N=C(C(C(N)=O)=N3)C)C=C2)CC1)=O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 367.45 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Floettmann E, Lees D, Seeliger F, Jones HB. Pharmacological inhibition of
DGAT1 induces sebaceous gland atrophy in mouse and dog skin while overt alopecia
is restricted to the mouse. Toxicol Pathol. 2015 Apr;43(3):376-83. doi:
10.1177/0192623314545657. Epub 2014 Aug 11. PubMed PMID: 25112279.


2: Denison H, Nilsson C, Löfgren L, Himmelmann A, Mårtensson G, Knutsson M,
Al-Shurbaji A, Tornqvist H, Eriksson JW. Diacylglycerol acyltransferase 1
inhibition with AZD7687 alters lipid handling and hormone secretion in the gut
with intolerable side effects: a randomized clinical trial. Diabetes Obes Metab.
2014 Apr;16(4):334-43. doi: 10.1111/dom.12221. Epub 2013 Oct 31. PubMed PMID:
24118885.


3: Barlind JG, Bauer UA, Birch AM, Birtles S, Buckett LK, Butlin RJ, Davies RD,
Eriksson JW, Hammond CD, Hovland R, Johannesson P, Johansson MJ, Kemmitt PD,
Lindmark BT, Morentin Gutierrez P, Noeske TA, Nordin A, O'Donnell CJ, Petersson
AU, Redzic A, Turnbull AV, Vinblad J. Design and optimization of
pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1)
leading to a clinical candidate dimethylpyrazinecarboxamide
phenylcyclohexylacetic acid (AZD7687). J Med Chem. 2012 Dec 13;55(23):10610-29.
doi: 10.1021/jm301296t. Epub 2012 Nov 21. PubMed PMID: 23116186.


4: Denison H, Nilsson C, Kujacic M, Löfgren L, Karlsson C, Knutsson M, Eriksson
JW. Proof of mechanism for the DGAT1 inhibitor AZD7687: results from a
first-time-in-human single-dose study. Diabetes Obes Metab. 2013
Feb;15(2):136-43. doi: 10.1111/dom.12002. Epub 2012 Sep 30. PubMed PMID:
22950654.